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Chemical Structure : CHMFL-KIT-031
Catalog No.: PC-62536Not For Human Use, Lab Use Only.
CHMFL-KIT-031 is a highly selective KIT kinase primary V559D mutant inhibitor with IC50/Kd of 28/266 nM, 10-20 fold selectivity over KIT wt.
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CHMFL-KIT-031 is a highly selective KIT kinase primary V559D mutant inhibitor with IC50/Kd of 28/266 nM, 10-20 fold selectivity over KIT wt.
CHMFL-KIT-031 also displays 15-400-fold selectivity over other primary mutants such as L576P and secondary mutants including T670I, V654A as well as N822K and D816V.
CHMFL-KIT-031 exhibits a selectivity S score (1) of 0.01 among 468 kinases/mutants in the KINOMEScan™ assay.
CHMFL-KIT-031 inhibits the proliferation of BaF3-TEL-KIT-V559D cells with IC50 of 25 nM, shows potent inhibitory efficacy for KIT V559D mediated signaling pathways in cell and anti-tumor activity in vivo.
| M.Wt | 487.516 | |
| Formula | C26H25N5O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Yu K, et al. Oncotarget. 2017 Nov 15;8(67):111110-111118.
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